Ramatroban, an orally bioavailable small molecule is a dual, reversible and potent antagonist of two G protein coupled receptors (i) Prostaglandin D2 (PGD2) receptor subtype DP2 (D prostanoid receptor 2; previously known as CRTH2) and (ii) thromboxane A2 (TxA2) receptors. Ramatroban (Baynas®, Bayer, Japan; dose: 50 mg and 75 mg tablets
Ramatroban, an orally bioavailable small molecule is a dual, reversible and potent antagonist of two G protein coupled receptors (i) Prostaglandin D2 (PGD2) receptor subtype DP2 (D prostanoid receptor 2; previously known as CRTH2) and (ii) thromboxane A2 (TxA2) receptors. Ramatroban (Baynas®, Bayer, Japan; dose: 50 mg and 75 mg tablets oral BID), also available as a generic from Kotobuki Pharma, Japan, has been safely and effectively used for the treatment of allergic rhinitis in Japan for the past 20 years. Thromboxane A2 and PGD2 play key roles in the pathogenesis of COVID-19 and the plasma levels of these lipid mediators are increased 5-10 fold in patients with COVID-19. (Prof. Srinivasa T. Reddy, UCLA; personal communication), even as the tissue expression of lipocalin-type PGD2 synthase and DP2 receptors are markedly increased. Ramatroban targets key pathogenic mechanisms and clinical stages in COVID-19.
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1) Archambault et al, medRxiv, 2020, doi: https://doi.org/10.1101/2020.12.04.20242115
2) Gupta and Chiang et al, Medical Hypothesis, 2020, doi: https://doi.org/10.1016/j.mehy.2020.110122
3) Gupta et al, J Mol Genet Med, 2020, doi: 10.37421/jmgm.2020.14.457
4) Chiang et al, SSRN, 2020, doi: http://dx.doi.org/10.2139/ssrn.3755292
5) Hottz et al
1) Archambault et al, medRxiv, 2020, doi: https://doi.org/10.1101/2020.12.04.20242115
2) Gupta and Chiang et al, Medical Hypothesis, 2020, doi: https://doi.org/10.1016/j.mehy.2020.110122
3) Gupta et al, J Mol Genet Med, 2020, doi: 10.37421/jmgm.2020.14.457
4) Chiang et al, SSRN, 2020, doi: http://dx.doi.org/10.2139/ssrn.3755292
5) Hottz et al, Blood, 2020, doi: https://doi.org/10.1182/blood.2020007252
6) Ackermann et al, NEJM, 2020, doi: https://doi.org/10.1056/NEJMoa2015432
Fibrosis, also known as fibrotic scarring, is a pathological wound healing that leads to considerable tissue remodeling and the formation of permanent scar tissue. There are many different types of fibrosis, including idiopathic pulmonary fibrosis, cirrhosis, cardiac fibrosis, renal fibrosis and more. The prevalence of idiopathic pulmonary fibrosis estimates in the USA varied between 14 and 27.9 cases per 100,000 population using narrow case definitions, and 42.7 and 63 per 100,000 population using broad case definitions. (Nalysnyk et al, 2012) Ramatroban is a promising treatment for fibrosis which affects the lives of millions of people.
COVID-19: As of December 2020, around 65 million people have been infection with COVID-19 and there has been over a million deaths. Evidence around the pathogenesis of COVID-19 is becoming clear. We need safe and effective drugs that are overly bioavailable and therefore practical in ambulatory patients since the majority of COVID-19 patients are outpatients. Currently, the focus is on anti-thrombotic and antiviral therapies. Ramatroban, also known as Elpidazo, is a potent reversible dual receptor antagonist of the thromboxane A2 and the prostaglandin D2 receptors that will serve as an anti-thrombotic and an immunomodulator in COVID-19.
Millions of children and adults globally and about 100,00 people in the US suffer from sickle cell disease (SCD). Many often develop painful vaso-occlusive crisis that diminish the quality of life and lead to mortality. The current FDA approved drugs for SCD are hydroxyurea, L-glutamine, crizanlizumab and voxelotor. Despite the recent advances, SCD patients remain at a high risk of developing fatal vascular complications driven by platelet activation. Ramatroban as a dual receptor antagonist of the DP2 and TP receptors can target platelet activation and treat thrombotic vasculopathy, thus improving survival of SCD patients. Ramatroban can target heme induced platelet activation by blocking CLEC2 signaling (Badolia et al, 2017) and reduce the thromboinflammatory state of SCD (Conran and De Paula, 2020). Visit changeforscd.com to learn more about the mechanisms of SCD.
Thrombosis is the formation of a blood clot inside a blood vessel, obstructing the flow of blood through the circulatory system. When a blood vessel is injured, the body uses platelets (thrombocytes) and fibrin to form a blood clot to prevent blood loss. Thrombosis can lead to stroke, myocardial infarction, limb ischemia, etc. Different types of thrombotic disorders include disseminated intravascular coagulation, deep venous thrombosis, venous thromboembolism, arterial thrombosis, pulmonary embolism, etc. Thrombosis can play a part in the pathogenesis of many conditions including viral and bacteria infections, and hematological disorders. Ramatroban is a promising treatment for thrombosis.
Cardiovascular disease describes a range of conditions that affect your cardiovascular system, especially with aging. This includes coronary artery disease, atherosclerosis, arrhythmias, congenital heart disease, cerebrovascular disease, myocardial infarction, etc. Ramatroban can potentially treat and prevent cardiovascular disease.
Ramatroban for healthy weight loss.
Vitamin K2
- Vitamin K2 activates proteins that promote bone formation and retard calcification and hardening of blood vessels.
- Vitamin K has been shown to prevent vascular calcification or hardening of the blood vessels, a serious complication of kidney disease.
Zinc
Zinc deficiency leads to:
- defects in immune system and infections
- loss of hair, taste, appetite
- Delayed wound healing
Note: Too much zinc can lead to copper deficiency. KidneyVite contains the right amount of zinc.
Copper
Copper deficiency leads to:
- anemia
- decrease in white blood cell count
- osteoporosis
- decreased ability to break down fat in the body
Selenium
Selenium deficiency leads to:
- Heart disease (cardiomyopathy)
- Anemia
- Myopathy, myositis
Lycopene
Lycopene deficiency leads to:
- Oxidative stress
- Inflammation
Lutein
Lutein deficiency leads to
- Heart disease and stroke
- Cataract and age-related macular degeneration
- Cancer at various sites
KidneyVite is the world's first complete multivitamin for kidney patients containing:
1. Active Folate (5-methy THF)
2. Vitamin K
3. Lycopene
4. Lutein
5. Other minerals (zinc, copper and selenium)
Unlike many other vitamin supplements, KidneyVite contains 5-methyl tetrahydrofolate.
Why 5-methyl tetrahydrofolate should replace folic acid:
1. For it to be active, synthetic folic acid needs conversion to 5 methyl THF by liver enzyme MTHFR.
2. The conversion is impaired when ‘T’ genotype of MTHFR is present.
3. 2 copies of ‘T’ genotype severely impair MTHFR enzyme activity and ‘TT’ may be present in up to nearly one-third of any population, depending on its race/ethnicity.
4. Unmetabolised folic acid is associated with immune suppression (↓ NK cells) and cancer.
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